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Cardiovascular Drugs during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Proprietary formulation of bretylium are no longer available but generic forms are. Bretylium is primarily indicated for life-threatening ventricular arrhythmias (e.g., ventricular tachycardia, ventricular fibrillation). No human data are published regarding safety of the drug during pregnancy. Bretylium was reported to be “without effect” in one rat study published by West (1962), but the relevance—if any—of this finding is unknown. It is an FDA category C drug.
Biochemical and Pharmacological Rationales in Radiotracer Design
Published in Lelio G. Colombetti, Principles of Radiopharmacology, 2019
Raymond E. Counsell, Nancy Korn
The report by Boura et al.45 that bretylium, an antiarrhythmic drug, was concentrated in the cat heart at early time periods after its administration prompted the synthesis of radioiodinated bretylium analogs (RIBA) as potential myocardial-scanning agents (Figure 4).46,47 Preliminary studies in rats using the ortho-isomer gave a greater ventricle/blood ratio than that reported for bretylium.47 Studies in dogs confirmed the ability of this compound to accumulate in myocardium and in sufficient concentration to obtain a scintigram.48 In dogs with experimentally induced infarctions, the ratio of radioactivity in normal vs. abnormal myocardium was sufficient to allow delineation of the infarction. Preliminary studies with normal human volunteers, however, were not successful in imaging the heart.49 This apparent species difference suggests that a nonhuman primate model may be necessary for preliminary testing of potential my-ocardial-imaging agents.
Halogen Labeled Compounds (F, Br, At, Cl) *
Published in Garimella V. S. Rayudu, Lelio G. Colombetti, Radiotracers for Medical Applications, 2019
Another approach to the incorporation of radiohalogens in a molecule is by isostere labeling. This approach is based on the electronic and steric consideration of the functional moieties. All the halogen elements are considered isosteres to one another, since they all contain the same numbers of electrons in the outer layers of orbitais. Substitution of I for Br in bretylium is one of the examples. Bretylium is an adrenergic neuron blocker. It was shown earlier to be taken up by the cat heart.46 This prompted the synthesis of the radioiodinated analog of bretylium by Counsell et al.47, 48 and it was found that this analog indeed concentrated in the heart of rats and dogs.
Efflux pump inhibitors as a promising adjunct therapy against drug resistant tuberculosis: a new strategy to revisit mycobacterial targets and repurpose old drugs
Published in Expert Review of Anti-infective Therapy, 2020
Liliana Rodrigues, Pedro Cravo, Miguel Viveiros
This strategy also identified several antiarrhythmic, antihypertensive drugs that potentially target a probable metal cation transporter P-type ATPase A CtpF (Rv1997) in M. tuberculosis. Deslanoside is a cardiac glycoside used to treat congestive heart failure, supraventricular arrhythmias and to control ventricular rate in the treatment of chronic atrial fibrillation. This compound inhibits the Na+/K+-ATPase pump, resulting in an increase in intracellular sodium and calcium concentrations that may promote activation of contractile proteins, such as actin and myosin [162]. Acetyldigitoxin is a cardioactive derivative of lanatoside A or of digitoxin used for fast digitalization in congestive heart failure. The proposed mode of action is similar to deslanoside: inhibition of the Na+/K+ pump that leads to increased amounts of calcium [163]. Ethacrynic acid is used in the treatment of high blood pressure and edema caused by diseases like congestive heart failure, liver failure, and kidney failure. It inhibits the symport of sodium, potassium, and chloride primarily in the ascending limb of Henle. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid [164]. Finally, the last drug in this group is bretylium, used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. The main mode of action for bretylium is thought to be inhibition of voltage-gated potassium channels and the Na+/K+-ATPase [165].